| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
The primary target of ABT-384 is 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). This enzyme catalyzes the conversion of inactive cortisone to active cortisol in tissues such as the liver and brain. By inhibiting 11β-HSD1, ABT-384 reduces the local production of cortisol, which is implicated in the pathophysiology of metabolic and cognitive disorders. It exhibits high affinity for 11β-HSD1 from various species, with Ki values in the range of 0.1-2.7 nM.
|
|---|---|
| ln Vitro |
In vitro, ABT-384 is a potent and selective inhibitor of 11β-HSD1. It exhibits high affinity for rodent, monkey, and human 11β-HSD1, with Ki values in the range of 0.1-2.7 nM. The compound's activity is characterized in enzyme assays measuring the conversion of cortisone to cortisol. Its selectivity over 11β-HSD2, the enzyme that converts cortisol to cortisone, is confirmed.
|
| ln Vivo |
In vivo, ABT-384 has been studied for its potential in treating Alzheimer's disease and major depressive disorder. By inhibiting 11β-HSD1, it blocks the regeneration of active cortisol, which may improve cognitive function and reduce depressive symptoms. The compound has progressed to Phase II clinical trials, indicating promising activity and safety in humans.
|
| Enzyme Assay |
In vitro enzyme assays for ABT-384 measure its inhibition of 11β-HSD1 activity. The enzyme is incubated with the substrate cortisone, and the conversion to cortisol is measured using techniques such as HPLC or mass spectrometry. The compound's Ki values are determined from dose-response curves. Selectivity over 11β-HSD2 is assessed by testing against this related enzyme.
|
| Cell Assay |
In vitro cell-based assays for ABT-384 evaluate its effects on cortisol production in cells. Cells expressing 11β-HSD1, such as hepatocytes or adipocytes, are treated with the compound, and the conversion of cortisone to cortisol is measured. The compound's ability to reduce cortisol production is assessed, and IC₅₀ values are determined.
|
| Animal Protocol |
In vivo animal studies for ABT-384 are conducted in models of metabolic and cognitive disorders. The compound is administered orally, and its effects on cortisol levels, glucose metabolism, and cognitive function are assessed. Efficacy studies are performed in models of Alzheimer's disease and depression. Pharmacokinetic studies determine the compound's half-life and bioavailability.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of ABT-384 have been characterized in preclinical and clinical studies. Its molecular weight is 493.56 g/mol. The compound is orally active and has progressed to Phase II clinical trials. Further details on its half-life, Cmax, and bioavailability are available from the primary research literature.
|
| Toxicity/Toxicokinetics |
The toxicity profile of ABT-384 has been evaluated in clinical trials. As a 11β-HSD1 inhibitor, its potential side effects may include adrenal insufficiency and electrolyte imbalance. The compound is for research use only and is not intended for human therapeutic applications without proper authorization.
|
| References |
|
| Additional Infomation |
ABT-384 has been used in trials investigating the treatment of Alzheimer's disease.
Additional information: ABT-384 is a potent, selective 11β-HSD1 inhibitor. It has high affinity for 11β-HSD1 from various species, with Ki values in the range of 0.1-2.7 nM. The compound has progressed to Phase II clinical trials for Alzheimer's disease. This product is for research use only and is not approved for clinical or therapeutic applications. |
| Molecular Formula |
C25H34F3N5O2
|
|---|---|
| Molecular Weight |
493.564976215363
|
| Exact Mass |
493.266
|
| Elemental Analysis |
C, 60.84; H, 6.94; F, 11.55; N, 14.19; O, 6.48
|
| CAS # |
868623-40-9
|
| PubChem CID |
11670435
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.6
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
35
|
| Complexity |
825
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CLHMYBJIOZXCEX-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C25H34F3N5O2/c1-23(2,33-7-5-32(6-8-33)19-4-3-18(14-30-19)25(26,27)28)22(35)31-20-16-9-15-10-17(20)13-24(11-15,12-16)21(29)34/h3-4,14-17,20H,5-13H2,1-2H3,(H2,29,34)(H,31,35)
|
| Chemical Name |
4-[[2-methyl-2-[4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]propanoyl]amino]adamantane-1-carboxamide
|
| Synonyms |
ABT 384 ABT384 ABT-384
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~31.25 mg/mL (~63.32 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.21 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0261 mL | 10.1303 mL | 20.2606 mL | |
| 5 mM | 0.4052 mL | 2.0261 mL | 4.0521 mL | |
| 10 mM | 0.2026 mL | 1.0130 mL | 2.0261 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01009216 | Completed | Drug: ABT-384 | Healthy | Abbott | 2009-10 | Phase 1 |
| NCT00968422 | Completed | Drug: ABT-384 Drug: Matching placebo to ABT-384 |
Healthy | Abbott | 2009-08 | Phase 1 |
| NCT01137526 | Completed | Drug: ABT-384 Drug: donepezil Drug: placebo |
Alzheimer's Disease | AbbVie (prior sponsor, Abbott) | 2010-05 | Phase 2 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
